scholarly journals HPTLC fingerprinting analysis and in vitro pharmacological activities of Hermannia geniculata roots phenols

2020 ◽  
Vol 5 (2) ◽  
pp. 13-23
Author(s):  
Adeniran Lateef Ariyo ◽  
Ashafa Anofi Omotayo Tom
Keyword(s):  
South African ◽  
Competitive Inhibition ◽  
Radical Scavenging ◽  
Retention Factor ◽  
Inhibitory Effect ◽  
Metallic Ions ◽  
Rf Values ◽  
Medicinal Properties ◽  
Layer Chromatography

AbstractHermannia geniculata is a herb that plays an important role in the treatment of an array of diseases including diabetes, ulcer, and colitis in the South African traditional medicine. The bioactive constituent and medicinal properties in phenols of Hermannia geniculata (PoHG) roots were investigated using high pressure thin layer chromatography (HPTLC). The α-amylase inhibitory potentials of PoHG was determined by reacting different concentration of the plant extract with 1% starch solution containing α-amylase. The inhibitory effect of the extract on α-glucosidase was evaluated by pre-incubating α-glucosidase with varying extract concentrations followed by the addition of ρ -nitrophenylglucopyranoside.. The reactive oxygen and free radical scavenging potentials of the extract were also analyzed. The result showed the presence of phenolic compounds in the extract with retention factor (Rf) values ranging from 0.14 to 095. The extract scavenged DPPH, ABTS+, hydroxyl, and superoxide anion radicals. The extract was able to chelate metallic ions with a lower IC50 value which differs significantly (p≤0.05) from silymarin. Moreover, PoHG extract inhibited the key enzymes (α-glucosidase and α-amylase) involved in carbohydrate catabolism with IC50 values of 1.76 ±0.14 and 7.52 ±0.23 mg/mL respectively while IC50 value reported for acarbose were 7.62 ±0.12 and 4.38 ±0.25 mg/mL for glucosidase and α-amylase, respectively. The α-glucosidase exhibited non-competitive inhibition by PoHG extract while α-amylase showed uncompetitive inhibition. This study confirmed the presence of phenol in PoHG extract and also showed an appreciable antioxidant and antidiabetic activities in vitro. Therefore, PoHG extract may be of nutraceutical importance.

scholarly journals Screening of in vitro antiviral activity of purified terpenoid extracts of selected sea weeds against chikungunya virus

2020 ◽  
pp. 320-324
Author(s):  
Sabira Siraj Sumayya ◽  
Abdulhadeef Shereefa Lubaina ◽  
Kumaraswamy Murugan
Keyword(s):  
Antiviral Activity ◽  
Chikungunya Virus ◽  
Kappaphycus Alvarezii ◽  
Inhibitory Effect ◽  
Hypnea Musciformis ◽  
High Incidence ◽  
Medicinal Properties ◽  
Inhibitory Potential ◽  
Layer Chromatography

Currently, the search of novel phytochemicals with unique biological potentialities is a pre-requisite for the designing ideal drugs for the human kind. Sea weeds are bioresources with a broad spectrum of medicinal properties with minimal side effects. Kerala, the Southern state of India reported high incidence of Chikungunya virus (CHIKV) infections in the last several tears. No specific virucidal therapy or effective vaccines are available. This emphasizes the need of searching for phytochemicals as drugs with less cost and more effective. Therefore, an attempt was made in screening purified terpenoid extracts of selected sea weeds as anti-CHIKV potential. In this study the terpenoids composition from the red algae Hypnea musciformis, Kappaphycus alvarezii and Gracillaria dura were identified and analyzed by thin layer chromatography and Gas chromatography- Mass spectrum. The methanolic extract of seaweeds was purified by column chromatography and each fraction was eluted by using petroleum ether and ethyl acetate as solvent combination. The analysis of the purified fraction of H. musciformis and K. alvarezii revealed the presence of 8 terpenoid fractions, and G. dura showed only 4 major components respectively. Vero cell lines were employed in the antiviral assays, infected to CHIKV, and treated with varied doses of purified terpenoid extracts. In the antiviral activity, terpenoid extracts of G. dura showed remarkable and promising EC50 inhibitory effect at 1.25 μg/ml. Further, the terpenoid extracts displayed efficient virucidal activity against CHIKV (inhibit around 90%) with 5 μg/ml dosage. As the last phase, terpenoid extracts added at time intervals of 0, 1, 2, 3 post-infection periods still maintained a significant inhibitory potential against CHIKV viral replication. Thus, the overall study suggests that the terpenoid extracts of G. dura may be effectively used in the prevention and treatment of CHIKV infections. Clinical studies may be warranted for designing a promising new anti-CHIKV drug.

scholarly journals PHARMACOGNOSTICAL SCREENING AND DETERMINATION OF ANTIOXIDANT ACTIVITY OF NELUMBO NUCIFERA GAERTN ETHANOL SEED EXTRACT BY DIFFERENT IN VITRO MODELS

2017 ◽  
Vol 9 (3) ◽  
pp. 64
Author(s):  
Alok Bhardwaj ◽  
Ketan P. Modi
Keyword(s):  
Antioxidant Activity ◽  
Thin Layer ◽  
Radical Scavenging ◽  
Seed Extract ◽  
Nelumbo Nucifera ◽  
Rf Values ◽  
Layer Chromatography ◽  
Radical Scavenging Assay

Objective: To perform the pharmacognostical screening and determination of antioxidant activity of Nelumbo nucifera Gaertn ethanol seed extract by different in vitro models.Methods: The different pharmacognostical parameters were evaluated as per standard protocols with some modifications. The various concentrations of ethanol seed extract of Nelumbo nucifera were evaluated for antioxidant activity using the standard in vitro methods like hydrogen peroxide (H2O2) scavenging assay, nitric oxide (NO) radical scavenging assay, reducing power capacity assessment, β-Carotene bleaching assay, ferric thiocyanate method (FTC) and thiobarbituric acid (TBA) assay.Results: Extractive values, ash values and moisture content values of Nelumbo nucifera were found to be as per the IP 2007 and Ayurvedic pharmacopoeia standard. Among the four extracts viz. Petroleum ether, chloroform, ethanol and aqueous, the ethanol extract showed significant antioxidant activity. The ethanol seed extract of Nelumbo nucifera (NNSE) exhibited high antioxidant activity (IC50 = 12.65 µg/ml) in 1, 1-diphenyl-2-picryldydrazyl (DPPH) radical scavenging assay. In FTC method the absorbance of NNSE increased slowly, which shows strong antioxidant ability. The thin layer chromatography (TLC) of the extract revealed 6 spots with the Rf values 0.41, 0.47, 0.59, 0.65, 0.67, 0.74 with the solvent system of toluene: ethyl acetate: formic acid (5:4:0.5, v/v/v). The high-performance thin layer chromatography (HPTLC) revealed the spots at Rf values 0.65 and 0.68. These fractions obtained by preparative TLC also confirmed the same. Conclusion: The present investigation suggested that the NNSE has significant antioxidant activity. These results clearly indicate that Nelumbo nucifera is effective against free radical mediated diseases, thus replacing the synthetic ones.

Effects of Dipyrone on Prostaglandin Production by Human Platelets and Cultured Bovine Aortic Endothelial Cells

1983 ◽  
Vol 49 (02) ◽  
pp. 132-137 ◽  
Author(s):  
A Eldor ◽  
G Polliack ◽  
I Vlodavsky ◽  
M Levy
Keyword(s):  
Endothelial Cells ◽  
Arachidonic Acid ◽  
Competitive Inhibition ◽  
Inhibitory Effect ◽  
Human Platelets ◽  
Ionophore A23187 ◽  
Aortic Endothelial Cells ◽  
Bovine Aortic Endothelial Cells ◽  
Aortic Endothelial

SummaryDipyrone and its metabolites 4-methylaminoantipyrine, 4-aminoantipyrine, 4-acetylaminoantipyrine and 4-formylaminoan- tipyrine inhibited the formation of thromboxane A2 (TXA2) during in vitro platelet aggregation induced by ADP, epinephrine, collagen, ionophore A23187 and arachidonic acid. Inhibition occurred after a short incubation (30–40 sec) and depended on the concentration of the drug or its metabolites and the aggregating agents. The minimal inhibitory concentration of dipyrone needed to completely block aggregation varied between individual donors, and related directly to the inherent capacity of their platelets to synthesize TXA2.Incubation of dipyrone with cultured bovine aortic endothelial cells resulted in a time and dose dependent inhibition of the release of prostacyclin (PGI2) into the culture medium. However, inhibition was abolished when the drug was removed from the culture, or when the cells were stimulated to produce PGI2 with either arachidonic acid or ionophore A23187.These results indicate that dipyrone exerts its inhibitory effect on prostaglandins synthesis by platelets or endothelial cells through a competitive inhibition of the cyclooxygenase system.

Curcumin-based antioxidant and glycohydrolase inhibitor compounds: Synthesis and in vitro appraisal of the dual activity against diabetes

2020 ◽  
Vol 16 ◽  
Author(s):  
Sajjad Esmaeili ◽  
Nazanin Ghobadi ◽  
Donya Nazari ◽  
Alireza Pourhossein ◽  
Hassan Rasouli ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Enzyme Inhibitor ◽  
Radical Scavenging Activity ◽  
Curcuma Longa ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Inhibitory Effect ◽  
Curcumin Derivatives ◽  
Reducing Power Assay

Background: Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. Objective: The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. Methods: Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH• ) radical scavenging activity were done to appraisal the antioxidant potential of these compounds in vitro. Results: Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). Conclusion: These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways.

scholarly journals Chemical Composition, In Vitro and In Silico Antioxidant Potential of Melissa officinalis subsp. officinalis Essential Oil

Antioxidants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1081
Author(s):  
Matilda Rădulescu ◽  
Călin Jianu ◽  
Alexandra Teodora Lukinich-Gruia ◽  
Marius Mioc ◽  
Alexandra Mioc ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Chemical Composition ◽  
Essential Oil ◽  
In Silico ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Melissa Officinalis ◽  
Β Carotene

The investigation aimed to study the in vitro and in silico antioxidant properties of Melissa officinalis subsp. officinalis essential oil (MOEO). The chemical composition of MOEO was determined using GC–MS analysis. Among 36 compounds identified in MOEO, the main were beta-cubebene (27.66%), beta-caryophyllene (27.41%), alpha-cadinene (4.72%), caryophyllene oxide (4.09%), and alpha-cadinol (4.07%), respectively. In vitro antioxidant properties of MOEO have been studied in 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging, and inhibition of β-carotene bleaching assays. The half-maximal inhibitory concentration (IC50) for the radical scavenging abilities of ABTS and DPPH were 1.225 ± 0.011 μg/mL and 14.015 ± 0.027 μg/mL, respectively, demonstrating good antioxidant activity. Moreover, MOEO exhibited a strong inhibitory effect (94.031 ± 0.082%) in the β-carotene bleaching assay by neutralizing hydroperoxides, responsible for the oxidation of highly unsaturated β-carotene. Furthermore, molecular docking showed that the MOEO components could exert an in vitro antioxidant activity through xanthine oxidoreductase inhibition. The most active structures are minor MOEO components (approximately 6%), among which the highest affinity for the target protein belongs to carvacrol.

scholarly journals GC-MS Based Identification of the Volatile Components of Six Astragalus Species from Uzbekistan and Their Biological Activity

Plants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 124
Author(s):  
Haidy A. Gad ◽  
Nilufar Z. Mamadalieva ◽  
Stefan Böhmdorfer ◽  
Thomas Rosenau ◽  
Gokhan Zengin ◽  
...  
Keyword(s):  
Radical Scavenging ◽  
Reducing Power ◽  
Principal Component ◽  
Inhibitory Effect ◽  
Maximum Activity ◽  
Volatile Components ◽  
Drug Candidates ◽  
Predominant Component ◽  
Clear Differentiation

The compositions of volatile components in the aerial parts of six Astragalus species, namely A. campylotrichus (Aca), A. chiwensis (Ach), A. lehmannianus (Ale), A. macronyx (Ama), A. mucidus (Amu) and A. sieversianus (Asi), were investigated using gas chromatograph-mass spectrometry (GC-MS) analysis. Ninety-seven metabolites were identified, accounting for 73.28, 87.03, 74.38, 87.93, 85.83, and 91.39% of Aca, Ach, Ale, Ama, Amu and Asi whole oils, respectively. Sylvestrene was the most predominant component in Asi, Amu and Ama, with highest concentration in Asi (64.64%). In addition, (E)-2-hexenal was present in a high percentage in both Ale and Ach (9.97 and 10.1%, respectively). GC-MS based metabolites were subjected to principal component analysis (PCA) and hierarchal cluster analysis (HCA) to explore the correlations between the six species. The PCA score plot displayed clear differentiation of all Astragalus species and a high correlation between the Amu and Ama species. The antioxidant activity was evaluated in vitro using various assays, phosphomolybdenum (PM), 2,2 diphenyl-1-picryl-hydrazyl-hydrate (DPPH), 2,2-azino bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cupric reducing antioxidant capacity (CUPRAC), ferric reducing power (FRAP) and ferrous ion chelation (FIC) assays. In addition, the potential for the volatile samples to inhibit both acetyl/butyrylcholinesterases (AChE, BChE), α- amylase, α-glucosidase and tyrosinase was assessed. Most of the species showed considerable antioxidant potential in the performed assays. In the DPPH assay, Ama exhibited the maximum activity (24.12 ± 2.24 mg TE/g sample), and the volatiles from Amu exhibited the highest activity (91.54 mgTE/g oil) in the ABTS radical scavenging assay. The effect was more evident in both CUPRAC and FRAP assays, where both Ale and Ama showed the strongest activity in comparison with the other tested species (84.06, 80.28 mgTE/g oil for CUPRAC and 49.47, 49.02 mgTE/g oil for FRAP, respectively). Asi demonstrated the strongest AChE (4.55 mg GALAE/g oil) and BChE (3.61 mg GALAE/g oil) inhibitory effect. Furthermore, the best tyrosinase inhibitory potential was observed for Ale (138.42 mg KAE/g). Accordingly, Astragalus species can be utilized as promising natural sources for many medicinally important components that could be tested as drug candidates for treating illnesses such as Alzheimer’s disease, diabetes mellitus and oxidative stress-related diseases.

Aqueous extracts of avocado pear (Persea americana Mill.) leaves and seeds exhibit anti-cholinesterases and antioxidant activities in vitro

2016 ◽  
Vol 27 (2) ◽  
Author(s):  
Ganiyu Oboh ◽  
Veronica O. Odubanjo ◽  
Fatai Bello ◽  
Ayokunle O. Ademosun ◽  
Sunday I. Oyeleye ◽  
...  
Keyword(s):  
Leaf Extract ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Seed Extract ◽  
Persea Americana ◽  
Dependent Manner ◽  
Natural Treatment

AbstractAvocado pear (The inhibitory effects of extracts on AChE and BChE activities and antioxidant potentials (inhibition of FeThe extracts inhibited AChE and BChE activities and prooxidant-induced TBARS production in a dose-dependent manner, with the seed extract having the highest inhibitory effect and the leaf extract exhibiting higher phenolic content and radical scavenging abilities, but lower Fe chelation ability compared with that of the seed. The phytochemical screening revealed the presence of saponins, alkaloids, and terpenoids in both extracts, whereas the total alkaloid profile was higher in the seed extract than in the leaf extract, as revealed by GC-FID.The anti-cholinesterase and antioxidant activities of avocado leaf and seed could be linked to their phytoconstituents and might be the possible mechanisms underlying their use as a cheap and natural treatment/management of AD. However, these extracts should be further investigated in vivo.

scholarly journals In vitro inhibitory effect of obtusofolin on the activity of CYP3A4, 2C9, and 2E1

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Na Liu ◽  
Ping Chen ◽  
Xiaojun Du ◽  
Junxia Sun ◽  
Shasha Han
Keyword(s):  
Human Liver ◽  
Competitive Inhibition ◽  
Liver Microsomes ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Cytochrome P450 Enzymes ◽  
Inhibition Model ◽  
Dose Dependent

Abstract Background Obtusofolin is the major active ingredient of Catsia tora L., which possesses the activity of improving eyesight and protecting the optic nerve. Investigation on the interaction of obtusofolin with cytochrome P450 enzymes (CYP450s) could provide a reference for the clinical application of obtusofolin. Methods The effect of obtusofolin on the activity of CYP450s was investigated in the presence of 100 μM obtusofolin in pooled human liver microsomes (HLMs) and fitted with the Lineweaver–Burk plots to characterize the specific inhibition model and kinetic parameters. Results Obtusofolin was found to significantly inhibited the activity of CYP3A4, 2C9, and 2E1. In the presence of 0, 2.5, 5, 10, 25, 50, and 100 μM obtusofolin, the inhibition of these CYP450s showed a dose-dependent manner with the IC50 values of 17.1 ± 0.25, 10.8 ± 0.13, and 15.5 ± 0.16 μM, respectively. The inhibition of CYP3A4 was best fitted with the non-competitive inhibition model with the Ki value of 8.82 μM. While the inhibition of CYP2C9 and 2E1 was competitive with the Ki values of 5.54 and 7.79 μM, respectively. After incubating for 0, 5, 10, 15, and 30 min, the inhibition of CYP3A4 was revealed to be time-dependent with the KI value of 4.87 μM− 1 and the Kinact value of 0.0515 min− 1. Conclusions The in vitro inhibitory effect of obtusofolin implying the potential drug-drug interaction between obtusofolin and corresponding substrates, which needs further in vivo validations.

scholarly journals Profile of Thin-Layer Chromatography and UV-Vis Spectrophotometry of Akar Kuning Stem Extract (Arcangelisia flava)

2018 ◽  
Vol 1 (2) ◽  
pp. 72-76 ◽  
Author(s):  
Mohammad Rizki Fadhil Pratama ◽  
Suratno Suratno ◽  
Evi Mulyani
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Ethanol Extract ◽  
Retention Factor ◽  
Polar Solvents ◽  
Central Kalimantan ◽  
Stem Extract ◽  
Rf Values ◽  
Layer Chromatography ◽  
Chloroform Methanol

This study aims to obtain the profile of Thin-Layer Chromatography (TLC) and Ultraviolet-Visible (UV-Vis) spectrophotometry from ethanol extract of akar kuning stems (Arcangelisia flava) from Central Kalimantan. The TLC method is used with the orientation phase of the combination of polar-non-polar solvents resulting from orientation, while ethanol is used as the solvent for UV-Vis spectrophotometers. TLC results showed the formation of 3 stains on a combination of polar solvents chloroform : methanol : water while in a non-polar solvent combination n-hexane : ethyl acetate did not show any stains. Comparison of retention factor (Rf) values show the best combination of polar solvents to separate stains at a ratio of 5 : 2 : 1, respectively. Separation in 2-dimensional TLC with polar solvents showed a similar pattern with 1-dimensional separation in the form of 3 stains. UV-Vis spectrophotometer results showed 4 main peaks with wavelength 227.2; 267.4; 345.2; and 425.3 nm, respectively. The profile of the peak formed is very similar to that shown by berberine, one of the main metabolites of akar kuning. TLC and UV-Vis spectrophotometers profiles obtained are expected to support further research using akar kuning stems, especially those from Central Kalimantan.

scholarly journals Nauclea latifolia Sm. Leaf Extracts Extenuates Free Radicals, Inflammation, and Diabetes-Linked Enzymes

2020 ◽  
Vol 2020 ◽  
pp. 1-13 ◽  
Author(s):  
Franklyn Nonso Iheagwam ◽  
Emmanuel Nsedu Israel ◽  
Kazeem Oyindamola Kayode ◽  
Opeyemi Christianah DeCampos ◽  
Olubanke Olujoke Ogunlana ◽  
...  
Keyword(s):  
Competitive Inhibition ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Peroxide Radical ◽  
Hypotonic Solution ◽  
Leaf Extracts ◽  
Inhibitory Activities ◽  
Anti Inflammatory ◽  
Nauclea Latifolia

This study was carried out to assess the in vitro antioxidant, anti-inflammatory and antidiabetic effects of Nauclea latifolia (Sm.) leaf extracts. Ethanolic (NLE) and aqueous (NLA) extract of N. latifolia leaves were prepared and assessed for their anti-inflammatory activity, antioxidant potential, α-amylase and α-glucosidase inhibitory activities, and the mechanism of enzyme inhibition in vitro using standard established methods. From the results, phytochemicals such as flavonoids, phenolics, glycosides, and tannins were detected in both extracts of N. latifolia with NLE having a significantly (p<0.05) higher phytochemical content. NLE displayed significantly (p<0.05) better total antioxidant capacity, reducing power, 2,2-diphenyl-2-picrylhydrazyl, and hydrogen peroxide radical scavenging activities. For anti-inflammatory activities, 70.54±2.45% albumin denaturation inhibition was observed for NLE while 68.05±1.03% was recorded for NLA. Likewise, 16.07±1.60 and 14.08±1.76% were obtained against hypotonic solution and heat-induced erythrocyte haemolysis, respectively, for NLE while 20.59±4.60 and 24.07±1.60% were respective NLA values. NLE (IC50: 4.20±0.18 and 1.19±0.11 mg/mL) and NLA (IC50: 11.21±0.35 and 2.64±0.48 mg/mL) α-glucosidase and α-amylase inhibitory activities were dose-dependent with uncompetitive and competitive inhibition elicited, respectively, by the extracts. A significant positive association (p<0.01 and 0.05) was identified between antioxidant activity and carbohydrate-metabolising enzyme inhibitory activity. The obtained result suggests N. latifolia leaf could serve as an alternative candidate for managing diabetes mellitus due to its antioxidant and anti-inflammatory association with diabetes-linked enzymes.

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